Solubilization of unilamellar liposomes by betaine-type zwitterionic/anionic surfactant systems

The mechanisms governing the solubilizing interactions between zwitterionic/anionic mixed surfactant systems at different molar fractions of the zwitterionic surfactant (X_zwitter) and neutral or electrically charged unilamellar liposomes were investigated. The mixed systems were formed by N-dodecyl-N,N-dimethylbetaine and sodium dodecyl sulfate in the presence of piperazine-1,4-bis-(2-ethanesulfonic acid) buffer at pH 7.20. Unilamellar liposomes formed by egg phosphatidylcholine, in some cases together with stearylamine or phosphatidic acid, were used. Solubilization was detected as a decrease in static light-scattering of liposomes. Two parameters were regarded as corresponding to the effective surfactant/lipid molar ratios (Re) at which the surfactant system (i) saturated the liposomes, Re_sat, and (ii) led to a total solubilization of liposomes, Re_sol. From these parameters the bilayer/aqueous medium surfactant partition coefficients for the saturation (K_sat) and complete bilayer solubilization (K_sol) were determined. When X_zwitter was 0.40, The Re and K parameters showed a maximum, whereas the critical micellar concentration (CMC) of these systems exhibited a minimum, regardless of the electrical charge of bilayers. Given that the ability of the surfactant systems to saturate or solubilize liposomes is inversely related to the Re_sat and Re_sol parameters, these capacities appear to be directly correlated with the CMC of the mixed systems. The similarity of both K_sat and K_sol (particularly for X_zwitter=0.2–0.8) suggests that a similar partition equilibrium governs both the saturation and the complete solubilization of bilayers, the free surfactant concentration (S_a,S_b), remaining almost constant with similar values to the CMC for each mixed system studied.     

环胞苷二棕榈酸酯脂质体粒度分布及微黏度的测定

对环胞苷二棕榈酸酯脂质体的物理稳定性进行了评价。用反相蒸发法制备环胞苷二棕榈酸酯脂质体,将其与空白脂质体对照,分别测定了它们受热前后的粒度分布及微黏度。结果表明,经37℃,40 h温育后其平均粒径仅增加了0.54μm,而空白脂质体增加了1.35μm。环胞苷二棕榈酸酯脂质体的微黏度比空白脂质体提高了近一倍。环胞苷二棕榈酸酯载于脂质体上提高了脂质体的物理稳定性。     

脂质体及其应用

综述了脂质体在医药制剂、化妆品中的应用状况和前景及其典型的制备方法。     

Antioxidant activity of grape extracts in a lecithin liposome system

Extracts of 14 different grapes were tested for their antioxidant activities in a copper-catalyzed lecithin liposome oxidation assay and analyzed for their phenolic components by high-performance liquid chromatography (HPLC). The total phenolic contents of the grape extracts varied from 176 to 1236 mg gallic acid equivalents (GAE)/L. Extracts of red wine grape varieties contained higher concentrations of phenolics than other varieties. When compared at the same 20 μM GAE basis, the grape extracts inhibited formation of conjugated diene hydroperoxides by 25.1 to 67.9%, and hexanal formation by 49.3 to 97.8%. Extracts of red table grape varieties Red Globe and Emperor and white wine grape varieties Chardonnay and Sauvignon Blanc gave the highest antioxidant activities. The relative percentage inhibition of conjugated dienes and hexanal correlated with total phenols (r=0.86 and 0.89). HPLC analyses showed that anthocyanins were the most abundant phenolic compounds in extracts of red grapes, and flavonols were most abundant in extracts of white grapes.     

HP-β-CD对脂质体和真核细胞通透性的影响

以薄膜水化法制备的阴离子脂质体的平均粒径为（180±2.3）nm．Zeta电位为-33．9mV．分别以脂质体中钙黄绿素的泄露量和紫外分光光度法测定蛋白含量,以表征羟丙基书-环糊精（HP-β-CD）对脂质体和真核微生物蓝色犁头霉（Absidiacoerulea）细胞通透性的影响．结果表明：在HP-f1．CD作用下,两者的通透性变化趋势一致．分析比较HP-β-CD作用下的甾体化合物17a,21-二羟基孕甾-4-烯-3,20-二酮（RS）在脂质体和菌体细胞中的通量变化的相关性,表明脂质体与细胞通量变化的拟合度达到97．9％,相关性显著（P〈0．05）．由此说明,本研究建立的脂质体制备方法以及获得的脂质体能够模拟真核细胞,应用于真核微生物的生物学研究．     

Adaptation of a Biomineralization Strategy for Remineralization of Enamel and Dentin

The bio- inspired strategy of triggered release of Ca^2＋ , Pi, F from prosomal compartments was used to induce rapid formation of FHA for potential dental use ： Calcium and inorganic phosphate salts were separately loaded into temperature-sensitive liposome composed of 90% DPPC and 10% DMPC. When heated from the room temperature to 35- 37 ℃ , the entrapped calcium, inorganic phosphate and fl~rin released from the liposome,A mixture of Ca- Pi and F-loaded liposome formed apatite. The mineral was indicated by a rapid drop in suspension PH from 7.4 approximately 6. This was illustrated by applying a liposome suspension warmed human dentin and enamel surface which resulted in deposition of apatite onto the tissue substrates.     

Improved physical stability of docosahexaenoic acid and eicosapentaenoic acid encapsulated using nanoliposome containing α‐tocopherol

This study aimed to develop a nanoliposomal formulation containing α‐tocopherol loaded with eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) and to characterise the formulation by its physical stability. For this purpose, different nanoliposomal formulations with dipalmitoyl phosphocholine were prepared using a modified thin‐film hydration method and evaluated by particle size, polydispersity index (PDI), transmission electron microscopy, differential scanning calorimetry and determining the encapsulation efficiencies of DHA and EPA. A physical stability study was conducted by investigating the change in the vesicle encapsulation efficiency, particle size, PDI and shape when stored at 4, 30 and 40 °C for 3 months. High encapsulation efficiency of DHA and EPA (89.1% ± 0.6% and 81.9% ± 1.4%) and appropriate particle size (82 ± 0.8 nm) were obtained for liposomes composed of α‐tocopherol. The optimum formulation was stable for 90 days when kept at 4 °C. This study demonstrated that α‐tocopherol had a protective effect on the physical stability of the nanoliposomes containing DHA and EPA.     

A novel insight to screen the optimal spray-drying protectants and parameters for manufacturing lactic acid bacteria preparations

Abstract

This study constructed a β-galactosidase (β-gal) liposome model instead of bacterial cells to optimize spray-drying protectants and parameters. The screened protectant combination consisted of 35?g/L monosodium glutamate, 50?g/L sucrose, and 35?g/L maltodextrin. The optimal parameters for spray drying were 130?°C inlet air temperature, 7.5?mL/min feed flow rate, and 150?mL optimal protectant combination. The viability of the five lactic acid bacteria strains spray-dried with the optimized protectant and parameters was over 50%. Lactobacillus helveticus strain LH-9’s mechanism of resistance to spray-dry treatment was investigated in the presence of the optimal protectant combination.     

含多重结构包覆载体技术的研究进展

概述了多重结构乳状液的结构类型、制备方法及其在药品、化妆品等领域的应用,综述了含多重结构的包覆载体,包括了脂质体、微胶囊和固体脂质纳米粒及其制备方法与研究现状,阐述了含多重结构的包覆载体的特性。     

以酒石酸为骨架的新型阳离子脂质材料的合成

以天然产物L-(+)-酒石酸为骨架,以氨基己酸、辛胺、十二胺或十六胺为原料成功构建了3种新型阳离子脂质材料。所得产物结构经~1HNMR、IR和质谱等进行了表征。结果表明,所得中间体和阳离子脂质材料的结构与目标化合物结构相符,为基因治疗中阳离子脂质体的制备提供了载体材料。